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Encapsulation Methods and Releasing Mechanisms of Encapsulated Active Drug 封装方法和封装活性药物的释放机制
Pub Date : 2024-01-15 DOI: 10.22270/jddt.v14i1.6356
Kakwokpo Clémence N’GUESSAN-GNAMAN, Nakognon Awa TUO-KOUASSI, Ismael Dally, Sandrine AKA-ANY-GRAH, Rosine Désirée CHOUGOUO KENGNE-NKUITCHOU, A. Lia, Apo Laurette Anin, Alain N’GUESSAN
Substances of plant origin are chemically unstable and easily oxidized by external conditions. However, they have to remain in their bioactive form when they are used in food, pharmaceutical, nutraceutical and cosmetic industries. Encapsulation method is an effective technique that should protect them preventing the degradation of these active substances and thus prevent them from losing their activities. In this review, the strategies for encapsulating plant substances and their preparation methods including emulsification, atomization, coaxial electrospray system, lyophilization, coacervation, in situ polymerization, melt extrusion, supercritical fluid technology, fluidized bed coating etc. were discussed. The release mechanisms of plant active substances were also presented. The choice of an appropriate encapsulation technique and wall material depends on the final use of the product and the processing conditions involved. The use of liposomes, ethosomes, phytosomes, emulsions, microspheres, microcapsules, solid lipid nanoparticles including formulations based on plant substances has enhanced their therapeutic effects. With the use of all these encapsulation systems, the formulation is delivered in a targeted manner, giving it an on-site effect, and the bioavailability of the formulation is also improved. With these new drug delivery systems, actives and extracts used in herbal formulations exhibit improved stability, sustained release from the formulation, protection against toxicity, and improved therapeutic efficacy. Keywords : nanoparticles, bioactive substance, formulation
植物来源的物质化学性质不稳定,很容易被外界条件氧化。然而,当它们被用于食品、制药、营养保健品和化妆品行业时,必须保持其生物活性形式。封装方法是一种有效的技术,可以防止这些活性物质降解,从而防止它们失去活性。本综述讨论了封装植物物质的策略及其制备方法,包括乳化、雾化、同轴电喷雾系统、冻干、共凝、原位聚合、熔融挤出、超临界流体技术、流化床包衣等。此外,还介绍了植物活性物质的释放机制。选择合适的封装技术和壁材取决于产品的最终用途和相关的加工条件。脂质体、乙脂质体、植物脂质体、乳剂、微球、微囊、固体脂质纳米颗粒(包括基于植物物质的制剂)的使用增强了其治疗效果。通过使用所有这些封装系统,可以有针对性地输送制剂,使其产生现场效应,同时还能提高制剂的生物利用度。有了这些新的给药系统,中草药制剂中使用的活性物质和提取物就会表现出更高的稳定性、从制剂中持续释放、抗毒性和治疗效果。关键词:纳米颗粒、生物活性物质、配方
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引用次数: 0
Qualitative Phytochemical Investigation and Acute Oral Toxicity Study on Ethanolic Extract of Curcuma longa Leaves 莪术叶乙醇提取物的定性植物化学调查和急性口服毒性研究
Pub Date : 2024-01-15 DOI: 10.22270/jddt.v14i1.6244
Pratima Chourasiya, Rekha Gour, Anant K. Patel
The study focused on evaluating the acute toxicity and phytochemical composition of Curcuma longa leaves using Swiss albino mice. The investigation involved a two-phase acute toxicity test, with doses up to 5000 mg/kg administered orally. The results indicated no toxicity at lower doses, while signs of weakness, salivation, and reduced movement were observed at 1600 mg/kg. Lethal effects were noted at 5000 mg/kg, establishing the LD50 at 2154.06 mg/kg. Phytochemical analysis revealed the presence of alkaloids, flavonoids, glycosides, tannins, and volatile oils in the ethanolic extract. The extract exhibited a 27.37% yield, characterized by a yellowish-orange color and a sticky consistency. This comprehensive investigation sheds light on both the acute toxicity profile and the diverse phytochemical components presents in Curcuma longa leaves. Keywords: Curcuma longa, Phytoconstituent, Acute oral toxicity, Lokes method.
研究重点是利用瑞士白化小鼠评估莪术叶的急性毒性和植物化学成分。调查包括两阶段急性毒性试验,口服剂量最高为 5000 毫克/千克。结果表明,低剂量时无毒性,而剂量为 1600 毫克/千克时,则会出现虚弱、流涎和活动减少的症状。在 5000 毫克/千克的剂量下出现了致死效应,半数致死剂量为 2154.06 毫克/千克。植物化学分析显示,乙醇提取物中含有生物碱、黄酮、苷、单宁和挥发油。提取物的收率为 27.37%,呈橘黄色,粘稠。这项综合研究揭示了莪术叶的急性毒性特征和多种植物化学成分。关键词莪术 植物成分 急性口服毒性 洛克斯法
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引用次数: 0
Adult Onset Still’s Disease in a Patient with Fever of Unknown Origin: A Rare Case 不明原因发热患者中的成人型斯蒂尔病:一个罕见病例
Pub Date : 2024-01-15 DOI: 10.22270/jddt.v14i1.6201
Silky Kumari, Subhankar Das, Sudha Kumari, Gyan Ranjan, Mahaprasad Barik, Ramya Ranjan Kanta, Somnath Nishad
Adult onset Still’s disease (AOSD) is a rare clinical entity with unknown etiology, characterized by arthritis, fever, evanescent rash, and other systemic presentations. AOSD generally does not overlap with other rheumatic diseases. AOSD is a diagnosis by exclusion, and it is one of the common causes of pyrexia of unknown origin (PUO) which can be life-threatening if mistreated. Although steroids are the first line of therapy, about 20%-30% of patients are refractory, intolerant, and or relapse during tapering or upon discontinuation of steroids. There are no clinical guidelines in treating such patients, which is challenging. Keywords:  Still’s disease, arthritis, fever, auto-inflammatory
成人斯蒂尔病(Adult onset Still's disease,AOSD)是一种病因不明的罕见临床病,以关节炎、发热、皮疹和其他全身症状为特征。AOSD 一般不会与其他风湿性疾病重叠。AOSD 是一种排除性诊断,也是不明原因发热(PUO)的常见病因之一,如果治疗不当,可能会危及生命。虽然类固醇是第一线治疗方法,但约有 20%-30% 的患者对类固醇难治、不耐受,或在逐渐减量或停用类固醇后复发。目前还没有治疗这类患者的临床指南,因此具有挑战性。关键词 斯蒂尔病、关节炎、发热、自身炎症性
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引用次数: 0
Formulation and In Vitro Evaluation of Niosomal Gel for The Topical Administration of Losartan Potassium 用于局部给药洛沙坦钾的 Niosomal 凝胶的制备和体外评估
Pub Date : 2024-01-15 DOI: 10.22270/jddt.v14i1.6366
Ruthika Ratna Veni Marri, Mandeti Nithisha, Mamidipalli Apurva, Raghavarapu Prasanthi, Tirunagari Mamatha
This study aims to develop and test a topical drug delivery system for antihypertensive activity using Losartan potassium-loaded niosomes. The niosomes were created using the traditional ether injection approach, with four formulations made using cholesterol as the lipid and varying quantities of surfactants such as span 80 and span 60. The different formulations underwent testing for FTIR, particle size, zeta potential, drug content, entrapment efficiency, and in vitro release. FTIR analysis revealed that the medication was incompatible with excipients. The study concludes by highlighting current obstacles and future possibilities for the development of niosomes as effective vehicles. Overall, this analysis provides insight into the potential of niosomes in medication delivery and encourages further research in this field. Keywords: Losartan potassium, Antihypertensive, Niosomes, Tween 80 and Span 20
本研究的目的是开发和测试一种局部给药系统,利用洛沙坦钾负载的niosomes来发挥抗高血压活性。采用传统的乙醚注射法制作了四种以胆固醇为脂质、不同数量的表面活性剂(如 span 80 和 span 60)的niosomes配方。对不同配方进行了傅立叶变换红外光谱、粒度、ZETA电位、药物含量、包埋效率和体外释放测试。傅立叶变换红外分析表明,药物与辅料不相容。研究最后强调了开发有效载体--niosomes 的当前障碍和未来可能性。总之,该分析深入揭示了niosomes在给药方面的潜力,并鼓励在该领域开展进一步研究。关键词洛沙坦钾 抗高血压 尼奥索姆 吐温 80 和 司盘 20
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引用次数: 0
Effect of ethanolic stem-bark extract of Blighia unijugata on body and organ weight, biochemistry, and hematology in Sprague-Dawley rats Blighia unijugata 的乙醇茎皮提取物对 Sprague-Dawley 大鼠体重和器官重量、生物化学和血液学的影响
Pub Date : 2024-01-15 DOI: 10.22270/jddt.v14i1.6370
Hope K Fiadjoe, G. Koffuor
Introduction: While the efficacy of Blighia unijugata against various conditions has been scientifically validated, very little is known of its safety in normal rats. This study aimed to assess the toxic effects of the ethanolic stem bark extract of Blighia unijugata (EBU) on body and organ weight, biochemistry, and hematology of Sprague Dawley rats following repeated oral administration. Method: Twenty (20) male Sprague-Dawley rats were randomly selected into four groups (n = 5) and administered distilled water or EBU at doses of 50, 100, or 200 mg/kg respectively for 28 days. For each group, percentage changes in body and organ weight, serum lipid profile, fasting blood glucose levels, liver, and kidney functions, and the various hematological variables were determined. Results: EBU treatment  (50-200 mg/kg body weight) caused no significant changes (p>0.05) in the body weight and the relative organ weight of the heart, kidney, and spleen. Similarly, no significant changes (p>0.05) were observed in the lipid profile (Total Cholesterol, Triglycerides, High-Density Lipoproteins, Low-Density Lipoproteins, and Very Low-Density Lipoproteins), fasting blood glucose, serum urea, creatinine, albumin, globulin, total protein, total bilirubin, alanine aminotransferase, aspartate aminotransferase, and the hematological measures, except for a significant reduction (p ≤ 0.05) in Alkaline Phosphatase after treatment with 200 mg/kg EBU. Conclusion: Overall, this investigation underscores that EBU administration did not cause significant effects on the evaluated parameters, suggesting relative safety within the experimental conditions. However, for potential clinical trials and human use, additional studies such as chronic toxicity assessments across diverse animal models and dosage ranges are recommended. Keywords: Blighia unijugata; biochemistry, hematology, body weight, organ weight
简介:Blighia unijugata对各种疾病的疗效已得到科学验证,但对其在正常大鼠体内的安全性却知之甚少。本研究旨在评估重复口服 Blighia unijugata(EBU)的乙醇茎皮提取物对 Sprague Dawley 大鼠的体重和器官重量、生物化学和血液学的毒性影响。研究方法将 20 只雄性 Sprague-Dawley 大鼠随机分为四组(n = 5),分别按 50、100 或 200 毫克/千克的剂量给它们服用蒸馏水或 EBU,连续服用 28 天。测定每组大鼠的体重和器官重量变化百分比、血清脂质概况、空腹血糖水平、肝脏和肾脏功能以及各种血液学变量。结果EBU 处理(50-200 毫克/千克体重)对体重以及心脏、肾脏和脾脏的相对器官重量没有引起显著变化(P>0.05)。同样,在血脂谱(总胆固醇、甘油三酯、高密度脂蛋白、低密度脂蛋白和极低密度脂蛋白)、空腹血糖、血清尿素、肌酐、白蛋白、球蛋白、总蛋白、总胆红素、丙氨酸氨基转移酶、天门冬氨酸氨基转移酶和血液学指标方面也未观察到明显变化(p>0.05),只是碱性磷酸酶显著降低(p ≤ 0.05)。结论:总之,这项调查强调,服用 EBU 不会对评估参数造成显著影响,表明在实验条件下是相对安全的。然而,对于潜在的临床试验和人体使用,建议进行更多的研究,如不同动物模型和剂量范围的慢性毒性评估。关键词昙花;生物化学;血液学;体重;器官重量
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引用次数: 0
Tenapanor-A Novel Approach for Management of Hyperphosphatemia in End Stage Renal Disease: A Clinical Study Aggregate Review Tenapanor--治疗终末期肾病高磷血症的新方法:临床研究综述
Pub Date : 2024-01-15 DOI: 10.22270/jddt.v14i1.6336
Leema Lobo, N. Kishore, Manjari Sharma
The critical importance of phosphate regulation in chronic kidney disease (CKD) has been well understood for decades. But new findings, frequently applicable to routine medical care, continue to evolve. Poor health outcomes, greater morbidity, lowered quality of life, and a higher death rate from cardiovascular disease are all linked to the development of CKD-bone mineral ailment. Increased blood phosphate levels are linked to an increased risk of mortality in hemodialysis patients due to changes in phosphate breakdown and declining renal function as CKD advances.In this setting, according to  CKD-mineral bone disease recommendations, it is critical to regulate serum phosphate  levels in patients with CKD-mineral bone problem. If dialysis and dietary intervention fail to control blood phosphate levels, the use of phosphate binders is advised. Although phosphate binders are successful in lowering blood phosphate levels by actively binding to dietary phosphate, certain individuals have adverse effects that may restrict their use.These medications also have a significant pill load, which might result in poor treatment compliance. Tenapanor, a novel medication, works by inhibiting the sodium/hydrogen exporter isoform 3 (NHE3), which lowers intestinal phosphate absorption primarily by decreasing passive paracellular phosphate flow. Tenapanor also reduces the expression of the sodium phosphorus 2b transport protein (NaPi2b), which limits active transcellular phosphate absorption compensation. This is considered to be more effective phosphorous absorption regulator and a better target for tailored medication therapy. This clinical study aggregate report explores the currently published studies that have evaluated Tenapanor for the treatment of hyperphosphatemia in end stage renal disease patients on haemodialysis. Keywords: Tenapanor, phosphate binding agents, hyperphosphatemia, chronic kidney disease, phosphate control, phosphate binders, phosphate absorption, phosphate absorbtion inhibitor.
几十年来,人们已经充分认识到磷酸盐调节在慢性肾脏病(CKD)中的极端重要性。但是,经常适用于常规医疗护理的新发现仍在不断发展。不良的健康状况、更高的发病率、更低的生活质量以及更高的心血管疾病死亡率都与慢性肾脏病--骨矿物质疾病的发展有关。在这种情况下,根据 CKD-骨矿物质疾病的建议,调节 CKD-骨矿物质疾病患者的血清磷酸盐水平至关重要。如果透析和饮食干预无法控制血磷水平,建议使用磷酸盐结合剂。虽然磷酸盐结合剂通过主动结合饮食中的磷酸盐来成功降低血磷水平,但某些人可能会因不良反应而限制其使用。Tenapanor是一种新型药物,它通过抑制钠/氢输出器同工酶3(NHE3)发挥作用,NHE3主要通过减少被动的细胞旁磷酸盐流来降低肠道对磷酸盐的吸收。Tenapanor 还能减少钠磷 2b 转运蛋白(NaPi2b)的表达,从而限制主动的跨细胞磷酸盐吸收补偿。这被认为是更有效的磷吸收调节剂,也是量身定制药物治疗的更好靶点。本临床研究汇总报告探讨了目前已发表的评估特纳帕诺治疗血液透析终末期肾病患者高磷血症的研究。关键词特纳帕诺 磷酸盐结合剂 高磷酸盐血症 慢性肾病 磷酸盐控制 磷酸盐结合剂 磷酸盐吸收 磷酸盐吸收抑制剂
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引用次数: 0
Preparation and Evaluation of Ketoprofen Loaded Mucoadhesive Microspheres 酮洛芬负载型粘胶微球的制备与评估
Pub Date : 2024-01-15 DOI: 10.22270/jddt.v14i1.6353
Suman Pattanayak, L. Kanthal, Tamanna Afnan, Shalini Shukla, P. Panda
The aim of the present study was to prepare and evaluate Ketoprofen loaded microspheres fabricated with sodium alginate and Carbopol 934 by ion gelation method which enhances the drug residence time into the stomach by adhering to the mucus layer of and control the rate of drug release for longer period of time. Ketoprofen is a nonsteroidal anti-inflammatory drug (NSAID) that is commonly used for its analgesic, anti-inflammatory, and antipyretic (fever-reducing) properties. It belongs to the propionic acid class of NSAIDs and is available in various formulations, including oral tablets, capsules, topical gels, creams, and as an injectable solution. In present study ketoprofen incorporates in mucoadhesive drug delivery system for utilizing its controlled drug delivery up to 12 hrs. In present study prepared microspheres were evaluated for- particle size, entrapment efficiency, percentage yield, morphology, mucoadhesive property, in-vitro drug release property. Keywords: Mucoadhesive microspheres, NSAID, ion gelation method, ketoprofen
本研究的目的是通过离子凝胶法制备和评估用海藻酸钠和 Carbopol 934 制成的酮洛芬负载微球,这种微球可通过粘附在胃黏膜层来延长药物在胃中的停留时间,并控制药物的释放速度。酮洛芬是一种非甾体抗炎药(NSAID),常用于镇痛、消炎和解热(退烧)。它属于丙酸类非甾体抗炎药,有多种剂型,包括口服片剂、胶囊、外用凝胶、乳膏和注射液。在本研究中,酮洛芬被纳入粘液黏附给药系统,用于控制给药时间长达 12 小时。本研究对制备的微球进行了粒度、包埋效率、产量百分比、形态、粘附性、体外药物释放性能等方面的评估。关键词黏附性微球 非甾体抗炎药 离子凝胶法 酮洛芬
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引用次数: 0
Preterm Birth: A Review of Its Early Diagnosis and Prevention 早产:早产的早期诊断和预防综述
Pub Date : 2024-01-15 DOI: 10.22270/jddt.v14i1.6372
Leena Muppa, K. Bhavadharini, A. Ramya, R. Bhavadharani
Preterm birth, a major global healthcare concern, is characterized by infants being born before completing 37 weeks of gestation. Accurate diagnosis and effective interventions are critical to managing this complex issue. This abstract provides an overview of the diagnosis and prevention of preterm birth, focusing on risk assessment, diagnostic techniques, and various interventions for mothers and newborns. The diagnostic process involves evaluating risk factors, clinical history, and the assessment of potential membrane rupture. Techniques such as speculum examination, the Nitrazine test, the Fern test, ultrasonography, and the Placental Alpha Microglobulin-1 test play vital roles in identifying membrane rupture and infection. Additional diagnostic markers include cervical ultrasonography and fetal fibronectin testing. Prevention strategies include lifestyle changes, maternal therapies, and antenatal interventions. Smoking cessation programs, low-dose aspirin, antenatal corticosteroid therapy, progesterone supplementation, magnesium sulfate, and antibiotic treatment are employed to reduce the risk of preterm birth. Cervical cerclage, another surgical intervention, is recommended in specific cases. For preterm newborns, immediate and effective care is vital. This includes thermal care, early breastfeeding, infection prevention, and respiratory distress syndrome management. These interventions are crucial in reducing infant mortality and morbidity associated with preterm birth. Efforts to diagnose and prevent preterm birth are essential in improving the well-being of both mothers and their newborns. A comprehensive approach, combining accurate diagnosis and effective interventions, can make a significant impact in reducing the burden of preterm birth on healthcare systems and families. Keywords: Preterm birth, infants, gestation, potential membrane rupture
早产是全球主要的医疗保健问题,其特点是婴儿在妊娠 37 周前出生。准确的诊断和有效的干预是处理这一复杂问题的关键。本摘要概述了早产的诊断和预防,重点是风险评估、诊断技术以及针对母亲和新生儿的各种干预措施。诊断过程包括评估风险因素、临床病史和潜在胎膜破裂的评估。窥器检查、硝肼试验、费恩试验、超声波检查和胎盘甲型微球蛋白-1 试验等技术在确定胎膜破裂和感染方面起着至关重要的作用。其他诊断指标包括宫颈超声波检查和胎儿纤维连接蛋白检测。预防策略包括改变生活方式、母体疗法和产前干预。戒烟计划、小剂量阿司匹林、产前皮质类固醇治疗、黄体酮补充剂、硫酸镁和抗生素治疗都可用于降低早产风险。在特殊情况下,建议采用宫颈环扎术(另一种手术干预)。对于早产新生儿,及时有效的护理至关重要。这包括热护理、早期母乳喂养、感染预防和呼吸窘迫综合症处理。这些干预措施对于降低与早产相关的婴儿死亡率和发病率至关重要。诊断和预防早产对改善母亲和新生儿的福祉至关重要。将准确诊断和有效干预结合起来的综合方法可在减轻早产对医疗系统和家庭造成的负担方面产生重大影响。关键词早产、婴儿、妊娠、潜在胎膜破裂
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引用次数: 0
Ethanolic Stem-Bark Extract of Blighia unijugata Possesses Anti-Hyperglycemic and Anti-Hyperlipidemic Activity in a Streptozotocin-Induced Diabetes Model Blighia unijugata 的茎皮乙醇提取物在链脲佐菌素诱导的糖尿病模型中具有抗高血糖和抗高血脂活性
Pub Date : 2024-01-15 DOI: 10.22270/jddt.v14i1.6369
Hope K Fiadjoe, G. Koffuor
Introduction: The global rise in the incidence of diabetes mellitus, particularly type 2 diabetes mellitus (T2DM), and its associated complications have become a public health threat. Besides hyperglycemia, hyperlipidemia has been associated with diabetes due to the defect in insulin secretion and/or action. Medicinal plants are being investigated to discover drug alternatives with better efficacies, lesser adverse effects, and cost-effectiveness. This work investigated the anti-hyperglycemic and anti-hyperlipidemic activity of ethanolic stem bark extract of Blighia unijugata (EBU) in streptozotocin (STZ)-induced diabetic Sprague- Dawley (SD) rats. Method: T2DM was induced in male SD rats by a single intraperitoneal injection of STZ (50 mg/kg in 0.1 M citrate buffer, pH 4.5) and confirmed 72 hours later. EBU (100 and 200 mg/kg) and glibenclamide (5 mg/kg) were administered orally to the diabetic rats (n = 5) for 28 days. The effect of the treatments on fasting blood glucose (FBG), lipid profile, atherogenic predictor indices, and body weight were assessed. Results: EBU treatments significantly reduced (p≤0.001) elevated blood glucose, total cholesterol, triglycerides, and Very Low-Density Lipoprotein cholesterol (VLDL-c, p≤0.001) but increased High-Density Lipoprotein cholesterol (HDL, p≤0.05) compared to the diabetic control. Also, all the atherogenic risk predictor indices were significantly reduced (p≤0.001). In addition, EBU treatment mitigated the significant weight loss (p≤0.01) associated with the diabetic state when compared to the normal control. Conclusion: These findings first report the anti-hyperglycemic, anti-hyperlipidemic, and anti-atherogenic properties of the stem bark of ethanolic extract of Blighia unijugata, and can be further studied and used as an anti-diabetic and anti-hyperlipidemic agent. Keywords: Blighia unijugata; hyperglycemia; atherogenic index; hyperlipidemia; diabetes
导言:全球糖尿病,尤其是 2 型糖尿病(T2DM)发病率的上升及其相关并发症已成为公共健康的威胁。除高血糖外,由于胰岛素分泌和/或作用的缺陷,高脂血症也与糖尿病有关。目前正在对药用植物进行研究,以发现疗效更好、不良反应更少、成本效益更高的药物替代品。这项工作研究的是 Blighia unijugata(EBU)茎皮乙醇提取物在链脲佐菌素(STZ)诱导的糖尿病 Sprague- Dawley(SD)大鼠中的抗高血糖和抗高血脂活性。研究方法给雄性 SD 大鼠腹腔注射一次 STZ(50 毫克/千克,0.1 兆柠檬酸缓冲液,pH 值为 4.5),诱发 T2DM,72 小时后确认。给糖尿病大鼠(n = 5)口服 EBU(100 和 200 mg/kg)和格列本脲(5 mg/kg)28 天。评估治疗对空腹血糖(FBG)、血脂概况、动脉粥样硬化预测指数和体重的影响。结果与糖尿病对照组相比,EBU 治疗能明显降低(p≤0.001)升高的血糖、总胆固醇、甘油三酯和极低密度脂蛋白胆固醇(VLDL-c,p≤0.001),但能增加高密度脂蛋白胆固醇(HDL,p≤0.05)。同时,所有动脉粥样硬化风险预测指数均显著降低(p≤0.001)。此外,与正常对照组相比,EBU 治疗减轻了与糖尿病状态相关的显著体重减轻(p≤0.01)。结论这些研究结果首次报道了白花蛇舌草乙醇提取物茎皮的抗高血糖、抗高血脂和抗动脉粥样硬化特性,可作为抗糖尿病和抗高血脂药物进一步研究和使用。关键词白花蛇舌草;高血糖;动脉粥样硬化指数;高脂血症;糖尿病
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引用次数: 0
Solubility enhancement of meloxicam by phospholipid complexation 磷脂复合物提高美洛昔康的溶解度
Pub Date : 2024-01-15 DOI: 10.22270/jddt.v14i1.6390
Vaibhav Bhadange, Pravin Kawtikwar, Supriya Jogdand, Ankita Kawtikwar
The best solubility enhancement approach is phospholipids complexation. It has been effectively employed by a number of writers to enhance the permeability, oral bioavailability, and solubility of several medicinal substances. The meloxicam is a member of BCS Class II, and because of its poor solubility and high permeability, its clinical application may have been constrained. Therefore, it is necessary to use a method that modifies the biopharmaceutical features. In this work, meloxicam, an NSAID with demonstrated anticancer action, was combined with phospholipid to increase its solubility. Utilizing solvent evaporation, the meloxicam phospholipid complex was produced. Particle size, zeta potential, SEM analysis, in vitro drug release, and solubility were assessed for the produced complex. The results obtained in this study showed the smaller particle size in nanometer range and physical stability with desired zeta potential. Meloxicam's prolonged release from the phospholipid complex is demonstrated by the in vitro drug release investigation.  The apparent solubility analysis of meloxicam phospholipid complex. Pure meloxicam showed that the drug's solubility was several times higher than that of the pure form. Hence in conclusion we can say that the phospholipid complexation could be the ideal method for solubility enhancement of drug like meloxicam. Keyword: Meloxicam, phospholipid complex, solubility, drug release
磷脂复合物是提高溶解度的最佳方法。许多学者已经有效地利用磷脂复配来提高多种药物的渗透性、口服生物利用度和溶解度。美洛昔康属于 BCS II 类药物,由于其溶解性差、渗透性高,临床应用可能受到限制。因此,有必要使用一种改变生物制药特征的方法。在这项研究中,一种具有抗癌作用的非甾体抗炎药美洛昔康与磷脂结合,以增加其溶解度。通过溶剂蒸发,生产出了美洛昔康磷脂复合物。对所制复合物的粒度、ZETA电位、SEM分析、体外药物释放和溶解度进行了评估。研究结果表明,美洛昔康磷脂复合物的粒径在纳米范围内较小,且具有理想的 zeta 电位和物理稳定性。体外药物释放研究表明,美洛昔康可从磷脂复合物中延长释放时间。 美洛昔康磷脂复合物的表观溶解度分析。纯美洛昔康的表观溶解度分析表明,该药物的溶解度是纯美洛昔康的数倍。因此,我们可以说磷脂复合物是提高美洛昔康等药物溶解度的理想方法。关键词:美洛昔康 磷脂复合物 溶解度 药物释放
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Journal of Drug Delivery and Therapeutics
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